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Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain.

ABSTRACT: The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse transcriptase-associated ribonuclease H (RNase H) are both selective targets for HIV-1 chemotherapy, and the identification of dual IN/RNase H inhibitors is an attractive strategy for new drug development. We newly synthesized pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNase H function of RT, confirming the possibility of developing dual HIV-1 IN/RNase H inhibitors and obtaining new information for the further development of more effective dual HIV-1 inhibitors.

SUBMITTER: Cuzzucoli Crucitti G

PROVIDER: S-EPMC7745740 | biostudies-literature | 2015 Feb

REPOSITORIES: biostudies-literature

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Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain.

Cuzzucoli Crucitti Giuliana G Métifiot Mathieu M Pescatori Luca L Messore Antonella A Madia Valentina Noemi VN Pupo Giovanni G Saccoliti Francesco F Scipione Luigi L Tortorella Silvano S Esposito Francesca F Corona Angela A Cadeddu Marta M Marchand Christophe C Pommier Yves Y Tramontano Enzo E Costi Roberta R Di Santo Roberto R

Journal of medicinal chemistry 20150211 4

The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse transcriptase-associated ribonuclease H (RNase H) are both selective targets for HIV-1 chemotherapy, and the identification of dual IN/RNase H inhibitors is an attractive strategy for new drug development. We newly synthesized pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RN ...[more]

PMID: 25629256

Dataset Information

Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain.

Publications

Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain.

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